I am a
Home I AM A Search Login

Papers of the Week

Papers: 28 May 2022 - 3 Jun 2022

Pharmacology/Drug Development

2022 Dec

J Enzyme Inhib Med Chem



4-(3-Alkyl/benzyl-guanidino)benzenesulfonamides as selective carbonic anhydrase VII inhibitors.


Abdoli M, Giovannuzzi S, Supuran CT, Žalubovskis R
J Enzyme Inhib Med Chem. 2022 Dec; 37(1):1568-1576.
PMID: 35635139.


The treatment of chronic neuropathic pain remains one of the most challenging of all neurological diseases and very much an art. There exists no consensus for the optimal management of this condition at the moment. Gaining inspiration from recent studies which pointed out the involvement of brain-associated carbonic anhydrase (CA, EC isoform VII in the pathology of various neurodegenerative diseases, which highlighted the relationship between selective inhibition of this isozyme and relieve of neuropathic pain, herein we report the synthesis and CA VII inhibitory activity of novel 4-(3-alkyl/benzyl-guanidino)benzenesulfonamides. Ten benzyl-substituted and five alkyl-substituted 4-guanidinobenzenesulfonamide derivatives were obtained, some of which (, , and ) exhibited satisfactory selectivity towards CA VII over CA I and II, with K-s in the subnanomolar range and good selectivity indexes for inhibiting the target versus the off-target isoforms.